Tamarixetin
Based on 2 publication(s) in Google Scholar
Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways.
For research use only. We do not sell to patients.
- Purity: 98.80%
- CAS No.: 603-61-2
- Formula: C16H12O7
- Molecular Weight:316.26
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Tamarixetin
MoreAll Endogenous Metabolite Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.63 μM
Compound: 3a
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Anticancer activity against human A549 cells by HTS assay
Anticancer activity against human A549 cells by HTS assay
|
[PMID: 25139569] |
| Calu-1 | IC50 |
24.95 μM
Compound: 3a
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Anticancer activity against human Calu1 cells by HTS assay
Anticancer activity against human Calu1 cells by HTS assay
|
[PMID: 25139569] |
| HeLa | IC50 |
1.81 μM
Compound: 3a
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Anticancer activity against human HeLa cells by HTS assay
Anticancer activity against human HeLa cells by HTS assay
|
[PMID: 25139569] |
| HOP-62 | IC50 |
9.93 μM
Compound: 3a
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Anticancer activity against human HOP62 cells by HTS assay
Anticancer activity against human HOP62 cells by HTS assay
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[PMID: 25139569] |
| LOX IMVI | IC50 |
>50 μM
Compound: 3a
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Anticancer activity against human LOXIMVI cells by HTS assay
Anticancer activity against human LOXIMVI cells by HTS assay
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[PMID: 25139569] |
| M14 | IC50 |
14.85 μM
Compound: 3a
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Anticancer activity against human M14 cells by HTS assay
Anticancer activity against human M14 cells by HTS assay
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[PMID: 25139569] |
| Monocyte | IC50 |
4.6 μM
Compound: tamarixetin
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Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
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[PMID: 8882428] |
| Monocyte | IC50 |
4.6 x 10-6 M
Compound: tamarixetin
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Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
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[PMID: 8882428] |
| NCI-H1299 | IC50 |
21.97 μM
Compound: 3a
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Anticancer activity against human H1299 cells by HTS assay
Anticancer activity against human H1299 cells by HTS assay
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[PMID: 25139569] |
| NCI-H157 | IC50 |
3.04 μM
Compound: 3a
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Anticancer activity against human NCI-H157 cells by HTS assay
Anticancer activity against human NCI-H157 cells by HTS assay
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[PMID: 25139569] |
| NCI-H1792 | IC50 |
4.06 μM
Compound: 3a
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Anticancer activity against human NCI-H1792 cells by HTS assay
Anticancer activity against human NCI-H1792 cells by HTS assay
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[PMID: 25139569] |
| NCI-H1944 | IC50 |
3.86 μM
Compound: 3a
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Anticancer activity against human NCI-H1944 cells by HTS assay
Anticancer activity against human NCI-H1944 cells by HTS assay
|
[PMID: 25139569] |
| NCI-H460 | IC50 |
4.45 μM
Compound: 3a
|
Anticancer activity against human H460 cells by HTS assay
Anticancer activity against human H460 cells by HTS assay
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[PMID: 25139569] |
| NCI-H522 | IC50 |
>50 μM
Compound: 3a
|
Anticancer activity against human NCI-H522 cells by HTS assay
Anticancer activity against human NCI-H522 cells by HTS assay
|
[PMID: 25139569] |
| Peritoneal macrophage | IC50 |
25 μM
Compound: kp21
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Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
|
[PMID: 27955927] |
| Vero | IC50 |
170.3 μg/mL
Compound: Tamarixetin
|
Cytotoxicity against african green monkey Vero cells by MTT assay
Cytotoxicity against african green monkey Vero cells by MTT assay
|
[PMID: 18855442] |
Tamarixetin (0-100 μM; 0-72 h) is cytotoxic to leukemia cells, inhibits cell proliferation, induces cell apoptosis and cell cycle arrest[1].
Tamarixetin (0-100 μM; 1 h) inhibits the hypertrophy of H9c2 cells and the production of ROS induced by Phenylephrine (HY-B0769) in a dose-dependent manner[2].
Tamarixetin (0-25 μM; 30 min) inhibits the secretion of various inflammatory cytokines, promotes the secretion of anti-inflammatory cytokine IL-10, and inhibits the phosphorylation of JNK1, p38 and Akt, COX-2 expression and IκBα degradation in mouse bone marrow dendritic cells treated with LPS (HY-D1056)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS (HY-D1056) treated mouse bone marrow dendritic cells
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Concentration:25 μM
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Incubation Time:30 min
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Result:Inhibited the phosphorylation of JNK1, p38, and Akt, the expression of COX-2, and the degradation of IκBα.
Tamarixetin (intraperitoneal injection; 1 mg/kg; single dose) has better anti-inflammatory properties, which is related to the increase of the immune cell population secreting IL-10 in mouse models of bacterial septicemia[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Transverse aortic constriction (TAC) mouse model[2]
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Dosage:0.2%
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Administration:Feed management; 6 weeks
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Result:Alleviated pressure‑overload‑induced cardiac hypertrophy in mice.
Attenuated cardiac fibrosis and apoptosis in pressure‑overloaded hearts.
Suppressed oxidative stress.
Negatively regulated NFAT nuclear translocation level.
Was able to the down-regulate the activation of PI3K/AKT signaling pathway in the heart after pressure overload.
Chemical Information
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CAS No. 603-61-2
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Appearance Solid
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Molecular Weight 316.26
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Formula C16H12O7
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Color Yellow to brown
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SMILES
O=C1C(O)=C(C2=CC=C(OC)C(O)=C2)OC3=CC(O)=CC(O)=C13
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Synonyms
4'-O-Methyl Quercetin
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
Integrated metabolomics and proteomics analysis elucidated the therapeutic effect of Huangkui Capsule on tacrolimus-induced chronic nephrotoxicity in rats. [Abstract]2026 Apr 6:360:121196. PMID: 41534748 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845
Solvent & Solubility
DMSO : 50 mg/mL (158.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nicolini F, et al. Induction of G2/M phase arrest and apoptosis by the flavonoid tamarixetin on human leukemia cells. Mol Carcinog. 2014 Dec;53(12):939-50. [Content Brief]
[2]. Fan C, et al. Tamarixetin protects against cardiac hypertrophy via inhibiting NFAT and AKT pathway. J Mol Histol. 2019 Aug;50(4):343-354. [Content Brief]
[3]. Park HJ, et al. Tamarixetin Exhibits Anti-inflammatory Activity and Prevents Bacterial Sepsis by Increasing IL-10 Production. J Nat Prod. 2018 Jun 22;81(6):1435-1443. [Content Brief]
[4]. Song W, et al. Tamarixetin Attenuated the Virulence of Staphylococcus aureus by Directly Targeting Caseinolytic Protease P. J Nat Prod. 2022 Aug 26;85(8):1936-1944. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1620 mL | 15.8098 mL | 31.6196 mL | 79.0489 mL |
| 5 mM | 0.6324 mL | 3.1620 mL | 6.3239 mL | 15.8098 mL | |
| 10 mM | 0.3162 mL | 1.5810 mL | 3.1620 mL | 7.9049 mL | |
| 15 mM | 0.2108 mL | 1.0540 mL | 2.1080 mL | 5.2699 mL | |
| 20 mM | 0.1581 mL | 0.7905 mL | 1.5810 mL | 3.9524 mL | |
| 25 mM | 0.1265 mL | 0.6324 mL | 1.2648 mL | 3.1620 mL | |
| 30 mM | 0.1054 mL | 0.5270 mL | 1.0540 mL | 2.6350 mL | |
| 40 mM | 0.0790 mL | 0.3952 mL | 0.7905 mL | 1.9762 mL | |
| 50 mM | 0.0632 mL | 0.3162 mL | 0.6324 mL | 1.5810 mL | |
| 60 mM | 0.0527 mL | 0.2635 mL | 0.5270 mL | 1.3175 mL | |
| 80 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9881 mL | |
| 100 mM | 0.0316 mL | 0.1581 mL | 0.3162 mL | 0.7905 mL |
- Tamarixetin
- 603-61-2
- 4'-O-Methyl Quercetin
- Endogenous Metabolite
- ClpP
- Bacterial
- Apoptosis
- Akt
- Interleukin Related
- COX
- JNK
- p38 MAPK
- Reactive Oxygen Species (ROS)
- Transverse aortic constriction (TAC) model
- leukemia cells
- H9c2 cells. mouse bone marrow dendritic cells
- bacterial septicemia model
- Inhibitor
- inhibitor
- inhibit